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21. 发明申请

US20110200536A1 CHELATORS, PARAMAGNETIC CHELATES THEREOF AND THEIR USE AS CONTRAST AGENTS IN MAGNETIC RESONANCE IMAGING (MRI) 审中-公开
标题翻译：引证文献，参考文献及其作为磁共振成像（MRI）的对比剂使用
公开(公告)号：US20110200536A1
公开(公告)日：2011-08-18
申请号：US12672117
申请日：2008-08-12
申请人： Harry John Wadsworth , Ian Martin Newington , Dennis O'shea
发明人： Harry John Wadsworth , Ian Martin Newington , Dennis O'shea
IPC分类号： A61K49/10 , C07D407/14 , C07D401/14 , C07D403/14 , C07K2/00 , C07K16/00 , A61P43/00 , C08F8/30 , C08F138/02 , B82Y5/00
CPC分类号： C07D213/69 , C07D309/40 , C07D401/14 , C07D405/14
摘要： The present invention relates to chelators, in particular to chelators which are capable of forming complexes, i.e. paramagnetic chelates, with paramagnetic metal ions. The invention also relates to said paramagnetic chelates, said paramagnetic chelates linked to other molecules and their use as contrast agents in magnetic resonance imaging (MRI).
摘要翻译：本发明涉及螯合剂，特别涉及能够与顺磁金属离子形成络合物即顺磁性螯合物的螯合剂。本发明还涉及所述顺磁性螯合物，所述顺磁性螯合物与其它分子连接，以及它们在磁共振成像（MRI）中作为造影剂的用途。

22. 发明申请

US20110190618A1 IMAGING NEUROINFLAMMATION 有权
标题翻译：成像神经炎症
公开(公告)号：US20110190618A1
公开(公告)日：2011-08-04
申请号：US13119450
申请日：2009-10-02
申请人： Harry John Wadsworth , Bo Shan , Dennis O' Shea , Joanna Marie Passmore , William John Trigg
发明人： Harry John Wadsworth , Bo Shan , Dennis O' Shea , Joanna Marie Passmore , William John Trigg
IPC分类号： A61B6/00 , C07D495/04 , A61K51/00 , A61B19/00
CPC分类号： C07D495/04 , A61K51/0446
摘要： The present invention concerns in vivo imaging and in particular in vivo imaging of the peripheral benzodiazepine receptor (PBR). A tetracyclic indole in vivo imaging agent is provided that binds with high affinity to PBR, has good uptake into the brain following administration, and which preferentially binds to tissues expressing higher levels of PBR. The present invention also provides a precursor compound useful in the synthesis of the in vivo imaging agent of the invention, as well as a method for synthesis of said in vivo imaging agent comprising use of said precursor compound, and a kit for carrying out said method. A cassette for the automated synthesis of the in vivo imaging agent is also provided. In addition, the invention provides a radiopharmaceutical composition comprising the in vivo imaging agent of the invention, as well as methods for the use of said in vivo imaging agent.
摘要翻译：本发明涉及体内成像，特别是周边苯二氮卓受体（PBR）的体内成像。提供四环吲哚体内显像剂，其以高亲和力与PBR结合，在给药后具有良好的摄入脑中，并优先结合表达较高水平的PBR的组织。本发明还提供了可用于合成本发明的体内显像剂的前体化合物，以及包含使用所述前体化合物的所述体内显像剂的合成方法和用于实施所述方法的试剂盒。还提供了用于体内成像剂的自动合成的盒。此外，本发明提供了包含本发明的体内显像剂的放射性药物组合物，以及使用所述体内显像剂的方法。

23. 发明申请

US20100056787A1 CHELATING AGENTS 失效
标题翻译：焊接剂
公开(公告)号：US20100056787A1
公开(公告)日：2010-03-04
申请号：US12521195
申请日：2008-01-11
申请人： Harry John Wadsworth , Ian Martin Newington , Clare L. Jones , Amanda Ewan , Dennis O'Sheo
发明人： Harry John Wadsworth , Ian Martin Newington , Clare L. Jones , Amanda Ewan , Dennis O'Sheo
IPC分类号： C07D213/89 , C07D213/69
CPC分类号： C07D213/81 , A61K49/103
摘要： The present invention relates to chelating agents, in particular to chelating agents which are capable of forming complexes with paramagnetic metal ions such as iron (III) and gadolinium (III). The invention also relates to the complexes formed and their use as MRI contrast agents.
摘要翻译：本发明涉及螯合剂，特别涉及能够与顺磁金属离子如铁（III）和钆（III）形成络合物的螯合剂。本发明还涉及形成的复合物及其作为MRI造影剂的用途。

24. 发明授权

US07115249B2 Solid-phase electrophilic fluorination 失效
标题翻译：固相亲电氟化
公开(公告)号：US07115249B2
公开(公告)日：2006-10-03
申请号：US10482542
申请日：2002-06-18
申请人： Sajinder Kaur Luthra , Frank Brady , Harry John Wadsworth
发明人： Sajinder Kaur Luthra , Frank Brady , Harry John Wadsworth
IPC分类号： A61K51/00 , A61M36/14
CPC分类号： C07C229/36 , A61K51/0406 , C07B59/00 , Y02P20/55
摘要： The invention relates to compounds of formula (I); wherein R1 and R2 independently selected from C1-6 alkyl; P1, P2, P3, and P4 are each independently hydrogen or a protecting group; and their use in the preparation of 18F-labelled 6-L-fluorodopa
摘要翻译：本发明涉及式（I）化合物; 其中R 1和R 2独立地选自C 1-6烷基; P 1，P 2，P 3，P 4和P 4各自独立地为氢或保护基; 以及它们在制备F-18F-标记的6-L-氟多巴达中的用途

25. 发明授权

US09481685B2 Imaging neuroinflammation 有权
标题翻译：成像神经炎症
公开(公告)号：US09481685B2
公开(公告)日：2016-11-01
申请号：US13119450
申请日：2009-10-02
申请人： Harry John Wadsworth , Bo Shan , Dennis O'Shea , Joanna Marie Passmore , William John Trigg
发明人： Harry John Wadsworth , Bo Shan , Dennis O'Shea , Joanna Marie Passmore , William John Trigg
IPC分类号： A61K51/00 , A61M36/14 , C07D495/04 , A61K51/04
CPC分类号： C07D495/04 , A61K51/0446
摘要： The present invention concerns in vivo imaging and in particular in vivo imaging of the peripheral benzodiazepine receptor (PBR). A tetracyclic indole in vivo imaging agent is provided that binds with high affinity to PBR, has good uptake into the brain following administration, and which preferentially binds to tissues expressing higher levels of PBR. The present invention also provides a precursor compound useful in the synthesis of the in vivo imaging agent of the invention, as well as a method for synthesis of said in vivo imaging agent comprising use of said precursor compound, and a kit for carrying out said method. A cassette for the automated synthesis of the in vivo imaging agent is also provided. In addition, the invention provides a radiopharmaceutical composition comprising the in vivo imaging agent of the invention, as well as methods for the use of said in vivo imaging agent.
摘要翻译：本发明涉及体内成像，特别是周边苯二氮卓受体（PBR）的体内成像。提供四环吲哚体内显像剂，其以高亲和力与PBR结合，在给药后具有良好的摄入脑中，并优先结合表达较高水平的PBR的组织。本发明还提供了可用于合成本发明的体内显像剂的前体化合物，以及包含使用所述前体化合物的所述体内显像剂的合成方法和用于实施所述方法的试剂盒。还提供了用于体内成像剂的自动合成的盒。此外，本发明提供了包含本发明的体内显像剂的放射性药物组合物，以及使用所述体内显像剂的方法。

26. 发明授权

US08501153B2 Active enantiomer 有权
标题翻译：活性对映异构体
公开(公告)号：US08501153B2
公开(公告)日：2013-08-06
申请号：US12880218
申请日：2010-09-13
申请人： Radha Achanath , Srinath Balaji , Afsal M. Kadavilpparampu Mohamed , Umamaheshwar Mokkapati , Steven Fairway , Dimitrios Mantzilas , Dennis O'Shea , William John Trigg , Harry John Wadsworth , Joanna Marie Passmore , Bo Shan
发明人： Radha Achanath , Srinath Balaji , Afsal M. Kadavilpparampu Mohamed , Umamaheshwar Mokkapati , Steven Fairway , Dimitrios Mantzilas , Dennis O'Shea , William John Trigg , Harry John Wadsworth , Joanna Marie Passmore , Bo Shan
IPC分类号： A61K51/00 , A61K36/14
CPC分类号： C07D209/94 , A61K51/0446 , A61K51/0455 , A61K51/0468 , C07B59/002 , C07B2200/05 , C07D209/88 , C07D295/192 , C07D401/06 , C07D495/04
摘要： The present invention provides a PET tracer that has improved properties for imaging the peripheral benzodiazepine receptor (PBR) as compared with known such PET tracers. The present invention also provides a precursor compound useful in the preparation of the PET tracer of the invention and methods for the preparation of said precursor compound and said PET tracer. Also provided by the present invention is a radiopharmaceutical composition comprising the PET tracer of the invention. Methods for using the PET tracer and the radiopharmaceutical composition are also provided.
摘要翻译：本发明提供了与已知的这种PET示踪剂相比具有改进的外周苯并二氮杂受体（PBR）成像的特性的PET示踪剂。本发明还提供了可用于制备本发明的PET示踪剂的前体化合物和用于制备所述前体化合物和所述PET示踪剂的方法。本发明还提供了包含本发明的PET示踪剂的放射性药物组合物。还提供了使用PET示踪剂和放射性药物组合物的方法。

27. 发明授权

US08475768B2 Paramagnetic chelates thereof and their use as contrast agents in magnetic resonance imaging (MRI) 失效
标题翻译：其磁性螯合物及其作为造影剂用于磁共振成像（MRI）
公开(公告)号：US08475768B2
公开(公告)日：2013-07-02
申请号：US12672113
申请日：2008-08-12
申请人： Oskar Axelsson , Harry John Wadsworth , Ian Martin Newington , Dennis O'Shea
发明人： Oskar Axelsson , Harry John Wadsworth , Ian Martin Newington , Dennis O'Shea
IPC分类号： A61B5/055 , C08G18/62 , C07D213/62
CPC分类号： C07D401/14 , C07D213/81 , C07D309/40 , C07D407/14
摘要： The present invention relates to chelators, in particular to chelators which are capable of forming complexes, i.e. paramagnetic chelates, with paramagnetic metal ions. The invention also relates to said paramagnetic chelates, said paramagnetic chelates linked to other molecules and their use as contrast agents in magnetic resonance imaging (MRI).
摘要翻译：本发明涉及螯合剂，特别涉及能够与顺磁金属离子形成络合物即顺磁性螯合物的螯合剂。本发明还涉及所述顺磁性螯合物，所述顺磁性螯合物与其它分子连接，以及它们在磁共振成像（MRI）中作为造影剂的用途。

28. 发明申请

US20120251447A1 RADIOIODINATED TROPANE DERIVATIVES 审中-公开
标题翻译：放射性衍生物衍生物
公开(公告)号：US20120251447A1
公开(公告)日：2012-10-04
申请号：US13513650
申请日：2010-12-21
申请人： Michelle Emma Avory , Harry John Wadsworth , Robert James Domett Nairne
发明人： Michelle Emma Avory , Harry John Wadsworth , Robert James Domett Nairne
IPC分类号： C07D451/02 , A61K51/04
CPC分类号： C07D451/02 , A61K51/0448 , A61K51/0455
摘要： The present invention provides novel radio iodinated tropanes incorporating triazole or isoxazole rings. Also provided are methods of preparation of said tropanes from functionalised tropane precursors, using click cycloaddition chemistry, as well as radiopharmaceutical compositions comprising such radio iodinated tropanes. The invention also provides in vivo imaging methods using the radio iodinated tropanes.
摘要翻译：本发明提供了掺入三唑或异恶唑环的新型放射性碘化托烷。还提供了使用点状环加成化学制备来自功能化的托烷前体的所述托烷的方法，以及包含这种放射性碘化托烷的放射性药物组合物的方法。本发明还提供了使用放射性碘化托烷的体内成像方法。

29. 发明授权

US08066974B2 Contrast agents 失效
标题翻译：对比剂
公开(公告)号：US08066974B2
公开(公告)日：2011-11-29
申请号：US12299794
申请日：2007-05-10
申请人： Duncan Wynn , Harry John Wadsworth , Ian Martin Newington
发明人： Duncan Wynn , Harry John Wadsworth , Ian Martin Newington
IPC分类号： A61K49/04
CPC分类号： C07C275/42 , A61K49/0433 , C07C271/28
摘要： The present invention relates to a class of compounds and to diagnostic compositions containing such compounds where the compounds are iodine containing compounds. More specifically the iodine containing compounds are chemical compounds containing an aliphatic central moiety containing urea or urethane functions allowing for the arrangement of three iodinated phenyl groups bound thereto. The invention also relates to the use of such diagnostic compositions as contrast agents in diagnostic imaging and in particular in X-ray imaging and to contrast media containing such compounds.
摘要翻译：本发明涉及一类化合物和含有这些化合物的诊断组合物，其中化合物是含碘化合物。更具体地，含碘化合物是含有含有脲或氨基甲酸酯官能团的脂族中心部分的化合物，其允许与其结合的三个碘化苯基的排列。本发明还涉及这种诊断组合物作为造影剂在诊断成像中的用途，特别是在X射线成像中以及含有这种化合物的造影剂的用途。

30. 发明授权

US07767796B2 N4 chelator conjugates 有权
标题翻译： N4螯合剂共轭物
公开(公告)号：US07767796B2
公开(公告)日：2010-08-03
申请号：US11572161
申请日：2005-07-19
申请人： Anthony Eamonn Storey , Harry John Wadsworth , Nigel Anthony Powell , Philip Duncanson
发明人： Anthony Eamonn Storey , Harry John Wadsworth , Nigel Anthony Powell , Philip Duncanson
IPC分类号： C07F13/00
CPC分类号： A61K51/0478 , A61K51/0497
摘要： The present invention provides tetra-amine chelator conjugates with biological targeting moieties, linked via a linker group and technetium complexes thereof as radiopharmaceuticals. The linker group is such that the chelator is mono-functionalized at the bridgehead position and provides both flexibility and a lack or aryl groups, to minimize lipophilicity and steric hulk. Protected versions of the chelators are provided which permit conjugation with a wide range of targeting molecules without interfering reactions with the amine nitrogens of the tetra-amine chelator. Syntheses of the functionalised chelators are described, together with bifunctional chelate precursors. Radiopharmaceutical compositions comprising the technetium metal complexes of the invention are described, together with non-radioactive kits for the preparation of such radiopharmaceuticals.
摘要翻译：本发明提供四胺螯合剂与生物靶向部分，通过连接基团和其锝络合物作为放射性药物连接。接头基团使得螯合剂在桥头位置被单官能化并且提供柔性和缺乏或芳基，以使亲脂性和空间巨大的最小化。提供了螯合剂的保护形式，其允许与宽范围的靶向分子缀合，而不与四胺螯合剂的胺氮化物发生干扰反应。描述了官能化螯合剂的合成以及双官能螯合物前体。本发明描述了包含本发明的锝金属络合物的放射性药物组合物，以及用于制备这种放射性药物的非放射性试剂盒。

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